Negative Allosteric Modulation of the µ-Opioid Receptor

DNA-encoded libraries from WuXi AppTec were used in a “steered” screening against either inactive or active μ-opioid receptors in parallel, to find novel negative allosteric modulators of this receptor. The molecule discovered via DEL screening not only shows direct and effective in vitro and in vivo potency, but also helps elucidate the mechanism of negative allosteric modulation of GPCRs. This discovery provides a potential therapeutic solution for conquering the current opioid overdose epidemic. We are honored to be part of this collaboration with our academic partner Brian K. Kobilka, Nobel laureate and Professor at Stanford University. Learn more about this novel research and access bioRxiv by clicking below.